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Assay Detail

CHEMBL4269481

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen intracellular amastigote harboring beta-galactosidase infected in mouse NIH/3T3 cells after 96 hrs by CPRG reagent based assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Confidence 1 — Organism
Curated By Intermediate

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.
Woodring JL, Behera R, Sharma A, Wiedeman J, Patel G, Singh B, Guyett P, Amata E, Erath J, Roncal N, Penn E, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP.
ACS Med Chem Lett (2018) 9 : 996 -1001
PubMed 30344906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 5.42 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285290 1 6.21
CHEMBL110 BENZNIDAZOLE 4.0 1 6.10
CHEMBL4281306 1 6.10
CHEMBL4289030 1 5.82
CHEMBL4283366 1 5.77
CHEMBL4284550 1 5.75
CHEMBL4290139 1 5.72
CHEMBL4280380 1 5.70
CHEMBL4283656 1 5.68
CHEMBL4280205 1 5.60
CHEMBL4277293 1 5.60
CHEMBL4279896 1 5.58
CHEMBL4284713 1 5.47
CHEMBL4291524 1 5.46
CHEMBL495979 1 5.43
CHEMBL4287935 1 5.30
CHEMBL4279771 1 5.10
CHEMBL4287808 1 5.09
CHEMBL4288115 1 5.02
CHEMBL4287195 1 4.92
CHEMBL4280687 1 4.89
CHEMBL4283836 1 4.72
CHEMBL4286712 1 4.52
CHEMBL4281134 1 4.51
CHEMBL4292440 1 -
CHEMBL4290423 1 -
CHEMBL4291341 1 -
CHEMBL4279460 1 -
CHEMBL4286008 1 -
CHEMBL4293909 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285290 EC50 = 610.0 nM 6.21
CHEMBL110 BENZNIDAZOLE EC50 = 790.0 nM 6.10
CHEMBL4281306 EC50 = 800.0 nM 6.10
CHEMBL4289030 EC50 = 1500.0 nM 5.82
CHEMBL4283366 EC50 = 1700.0 nM 5.77
CHEMBL4284550 EC50 = 1800.0 nM 5.75
CHEMBL4290139 EC50 = 1900.0 nM 5.72
CHEMBL4280380 EC50 = 2000.0 nM 5.70
CHEMBL4283656 EC50 = 2100.0 nM 5.68
CHEMBL4277293 EC50 = 2500.0 nM 5.60
CHEMBL4280205 EC50 = 2500.0 nM 5.60
CHEMBL4279896 EC50 = 2600.0 nM 5.58
CHEMBL4284713 EC50 = 3400.0 nM 5.47
CHEMBL4291524 EC50 = 3500.0 nM 5.46
CHEMBL495979 EC50 = 3700.0 nM 5.43
CHEMBL4287935 EC50 = 5000.0 nM 5.30
CHEMBL4279771 EC50 = 8000.0 nM 5.10
CHEMBL4287808 EC50 = 8200.0 nM 5.09
CHEMBL4288115 EC50 = 9600.0 nM 5.02
CHEMBL4287195 EC50 = 12000.0 nM 4.92
CHEMBL4280687 EC50 = 13000.0 nM 4.89
CHEMBL4283836 EC50 = 19000.0 nM 4.72
CHEMBL4286712 EC50 = 30000.0 nM 4.52
CHEMBL4281134 EC50 = 30700.0 nM 4.51
CHEMBL4291210 EC50 > 50000.0 nM -
CHEMBL4294610 EC50 > 50000.0 nM -
CHEMBL4279269 EC50 > 50000.0 nM -
CHEMBL4293105 EC50 > 50000.0 nM -
CHEMBL4294413 EC50 > 50000.0 nM -
CHEMBL4291924 EC50 - -
CHEMBL4293909 EC50 > 50000.0 nM -
CHEMBL4286008 EC50 > 50000.0 nM -
CHEMBL4279460 EC50 > 50000.0 nM -
CHEMBL4291341 EC50 > 50000.0 nM -
CHEMBL4290423 EC50 > 50000.0 nM -
CHEMBL4292440 EC50 - -